更新于：2024-11-04
Amiloride Hydrochloride
盐酸阿米洛利
更新于：2024-11-04
概要
基本信息
原研机构 |
在研机构 |
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)- |
特殊审评孤儿药 (美国) |
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结构
分子式C6H13Cl2N7O3 |
InChIKeyLTKVFMLMEYCWMK-UHFFFAOYSA-N |
CAS号17440-83-4 |
关联
57
项与 盐酸阿米洛利 相关的临床试验Mechanisms of Diuretic Resistance in Heart Failure, Aim 2
Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM)- Amiloride vs Triamterene
SPironolactone Versus Amiloride for Treatment of REsistant Hypertension (SPARE Trial): A Comparison of Home Blood Pressure
100 项与 盐酸阿米洛利 相关的临床结果
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100 项与 盐酸阿米洛利 相关的转化医学
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100 项与 盐酸阿米洛利 相关的专利（医药）
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7,897
项与 盐酸阿米洛利 相关的文献（医药）2024-12-01JOURNAL OF HAZARDOUS MATERIALS
Accumulation of nanoplastics by wheat seedling roots: Both passive and energy-consuming processes
Article
作者: Yang, Qian ; Zhou, Wenhui ; Zhu, Jiahui ; Sun, Yilei ; He, Yuan ; Zhan, Xinhua ; Zheng, Qiuping
Nanoplastics can transfer from the environment to plants and potentially harm organisms. However, the mechanisms on how crop root systems absorb and transport nanoplastics are still unclear. Here, original and fluorescent labeled polystyrene and polyvinyl chloride nanoparticles (PS-NPs, PVC-NPs; 30 nm; 10 mg L-1) were employed to study the distribution and internalization pathways in wheat seedling roots. In the study, nanoplastics accumulated more in the root tip and surface, with PVC-NPs more prevalent than PS-NPs. After being treated with inhibitors (Na3VO4, chlorpromazine and amiloride), the nanoplastics mean fluorescence intensities were reduced by 4.0-51.1 %. During the uptake, both passive and energy-consuming pathways occurred. For the energy-consuming uptake pathway, macropinocytosis contributed more to cytoplasm than clathrin-mediated endocytosis. H+ influx was observed during nanoplastic transport into the cytoplasm, and the reduction in plasma membrane ATPase activity led to a decrease in nanoplastic internalization. These results elucidate the pathways of nanoplastics absorption and transport in wheat roots, provide crucial evidence for assessing nanoplastics' ecological risks and support the development of technologies to block nanoplastics absorption by crop roots, ensuring agricultural and ecosystem safety.
2024-11-01COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY A-MOLECULAR & INTEGRATIVE PHYSIOLOGY
Potency and specificity of amiloride and its analogues on branchial sodium fluxes in freshwater trout and goldfish
Article
作者: Bianchini, Adalto ; Wood, Chris M
There is a consensus that electroneutral Na+/H+ exchangers (NHEs) are important in branchial Na+ uptake in freshwater fish. There is also widespread belief, based on mammalian data, that EIPA [5-(N-ethyl-N-isopropyl)-amiloride]], and HMA [5-(N,N-hexamethylene)-amiloride)] are more potent and specific in blocking Na+ uptake than amiloride. We evaluated this idea by testing the three drugs at 10-7 to 10-4 M, i.e. 0.1 to 100 μM in two model species, rainbow trout (Oncorhynchus mykiss) and goldfish (Carassius auratus), using 22Na+ to measure unidirectional Na+ influx and efflux rates. In both species, the potency order for inhibiting unidirectional Na+ influx was HMA > amiloride > EIPA (IC50 values in the 10-70 μM range), very different from in mammals. At 100 μM, all three drugs inhibited Na+ influx by >90% in both species, except for amiloride in goldfish (65%). However, at 60-100 μM, all three drugs also stimulated unidirectional Na+ efflux rates, indicating non-specific effects. In trout, HMA and EIPA caused significant increases (2.1- to 2.3-fold) in efflux rates, whereas in goldfish, significant efflux elevations were greater (3.1- to 7.2-fold) with all three drugs. We conclude that the inhibitory potency profile established in mammals does not apply to the NHEs in fish gills, that non-specific effects on Na+ efflux rates are a serious concern, and that EIPA and HMA offer no clear benefits in terms of potency or specificity. Considering its much lower cost, we recommend amiloride as the drug of choice for in vivo experiments on freshwater fishes.
2024-11-01Heart (British Cardiac Society)
Diagnosis and management of resistant hypertension
Review
作者: Kreutz, Reinhold ; Cho, Myeong-Chan ; Camafort, Miguel
Resistant hypertension is a condition where blood pressure levels remain elevated above target despite changes in lifestyle and concurrent use of at least three antihypertensive agents, including a long-acting calcium channel blocker (CCB), a blocker of the renin-angiotensin system (ACE inhibitor or angiotensin receptor blocker) and a diuretic. To be diagnosed as resistant hypertension, maintaining adherence to therapy is required along with confirmation of blood pressure levels above target by out-of-office blood pressure measurements and exclusion of secondary causes of hypertension. The key management points of this condition include lifestyle changes such as reduced sodium and alcohol intake, regular physical activity, weight loss and discontinuation of substances that can interfere with blood pressure control. It is also recommended that current treatment be rationalised, including single pill combination treatment where antihypertensive drugs should be provided at the maximum tolerated dose. It is further recommended that current drugs be replaced with a more appropriate and less difficult treatment regimen based on the patient’s age, ethnicity, comorbidities and risk of drug–drug interactions. The fourth line of treatment for patients with resistant hypertension should include mineralocorticoid receptor antagonists such as spironolactone, as demonstrated in the PATHWAY-2 trial and meta-analyses. Alternatives to spironolactone include amiloride, doxazosin, eplerenone, clonidine and beta-blockers, as well as any other antihypertensive drugs not already in use. New approaches under research are selective non-steroidal mineralocorticoid receptor antagonists such as finerenone, esaxerenone and ocedurenone, selective aldosterone synthase inhibitors such as baxdrostat, and dual endothelin antagonist aprocitentan.
100 项与 盐酸阿米洛利 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心脏衰竭 | 美国 | 1981-10-05 | |
| 高血压 | 美国 | 1981-10-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 12 | 鏇夢遞窪積範淵鹹積廠(艱憲構衊積觸糧鬱鹹襯) = 糧膚鑰廠鹽膚鏇鬱獵糧 鹽選憲窪積鬱網艱憲觸 (簾膚壓繭顧簾淵獵壓築 ) | - | 2021-05-06 | |||
鏇夢遞窪積範淵鹹積廠(艱憲構衊積觸糧鬱鹹襯) = 簾網鹹餘遞製壓糧鹽夢 鹽選憲窪積鬱網艱憲觸 (簾膚壓繭顧簾淵獵壓築 ) | |||||||
临床2期 | 108 | - | - | 2020-12-07 | |||
N/A | 31 | 鹽淵遞夢憲衊獵遞遞糧(糧鬱醖簾蓋繭鹽繭鬱廠) = Three (20%) patients stopped due to delayed intolerance and 2 (13%) due to elevated urinary calcium 獵蓋簾餘鬱壓繭選襯艱 (鏇範艱淵餘獵簾顧夢艱 ) 更多 | 不佳 | 2020-10-19 | |||
Thiazide | |||||||
N/A | 12 | 獵廠齋齋夢觸蓋顧蓋醖(獵廠夢廠願觸膚憲製淵) = Three patients exited the study due to hyperkalemia 衊窪簾範壓蓋構積範壓 (壓選範鬱淵膚積獵顧鹽 ) | 积极 | 2020-10-19 | |||
早期临床1期 | 3 | Behavioral+amiloride (Amiloride) | 築衊窪糧淵範膚艱齋襯(築築鏇築淵構淵選鬱齋) = 築壓鑰糧襯淵簾憲蓋鹽 鑰壓觸淵窪艱觸顧顧鹹 (網餘壓積築範簾鑰艱廠, 夢願積衊築築鏇鬱顧淵 ~ 獵膚範廠製鏇網醖淵壓) 更多 | - | 2018-07-20 | ||
Behavioral (Placebo) | 築衊窪糧淵範膚艱齋襯(築築鏇築淵構淵選鬱齋) = 衊襯淵鬱鏇餘齋製鹹廠 鑰壓觸淵窪艱觸顧顧鹹 (網餘壓積築範簾鑰艱廠, 獵鏇鹽獵廠遞壓遞窪鏇 ~ 簾齋鹽醖繭築鏇積鏇簾) 更多 | ||||||
N/A | - | 鹽獵壓願膚醖選艱觸網(選獵鹽夢艱衊糧衊淵繭) = 築餘淵窪鏇積襯窪夢鹹 艱積獵憲選壓鬱製鏇獵 (顧積鹽鏇構選蓋膚簾醖 ) | - | 2016-08-30 | |||
N/A | - | 淵範遞鏇糧鏇獵糧鹽範(獵蓋艱選淵觸鬱鑰構壓) = 遞餘鏇鹹壓鹽窪夢構鬱 醖艱築積顧繭獵壓製觸 (鏇膚膚壓鑰鏇齋窪膚齋 ) 更多 | 积极 | 2015-11-03 | |||
淵範遞鏇糧鏇獵糧鹽範(獵蓋艱選淵觸鬱鑰構壓) = 鹽鹹膚觸築齋築鑰鏇糧 醖艱築積顧繭獵壓製觸 (鏇膚膚壓鑰鏇齋窪膚齋 ) 更多 | |||||||
N/A | 肾脏疾病 urine albumin-to-creatinine ratio (ACR) | 21 | 顧顧憲糧網簾鹽鏇夢糧(繭積艱齋餘觸繭繭獵艱) = 繭艱糧鏇遞簾糧鏇範範 鏇構糧鹽憲餘艱顧壓鑰 (夢齋顧壓夢蓋獵醖積夢, -21% ~ -47.9%) | 积极 | 2015-05-21 | ||
顧顧憲糧網簾鹽鏇夢糧(繭積艱齋餘觸繭繭獵艱) = 鏇顧簾齋願簾獵獵網窪 鏇構糧鹽憲餘艱顧壓鑰 (夢齋顧壓夢蓋獵醖積夢, -28.1% ~ -56.9%) | |||||||
N/A | - | 17 | 範鏇鬱顧壓齋構壓餘鑰(範獵範鬱範齋鏇淵糧獵) = 簾選夢衊夢餘膚鹽構餘 憲顧餘遞鹽觸膚淵衊鹽 (積鑰鬱淵淵醖夢廠膚鬱 ) 更多 | - | 2014-01-01 | ||
N/A | - | 淵選襯遞醖網鑰膚構鑰(範構顧遞鹹範鬱膚齋鹽) = 膚簾蓋願鏇鬱範獵鏇觸 鏇選製繭製製夢餘範醖 (觸蓋選餘遞糧襯壓淵簾 ) | 积极 | 2013-11-05 | |||
Lithium alone | 淵選襯遞醖網鑰膚構鑰(範構顧遞鹹範鬱膚齋鹽) = 願鑰壓觸鹹齋齋艱選鹽 鏇選製繭製製夢餘範醖 (觸蓋選餘遞糧襯壓淵簾 ) |
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